Key result
Most ACE-inhibitory peptides fail to activate ACE2, although specific peptides demonstrate antihypertensive activity.
Why the study?
Given structural similarities and interconnected cardiovascular roles of ACE and ACE2, this study investigated whether ACE-inhibitory peptides can also activate ACE2.
Does oral administration of ACE-inhibitory peptides activate ACE2 and lower blood pressure in spontaneously hypertensive rats?
Does oral administration of ACE-inhibitory peptides activate ACE2 and lower blood pressure in spontaneously hypertensive rats?
ACE2 activation is not a universal feature of ACE-inhibitory peptides, although specific peptides like IKW and RIY can activate ACE2 and lower blood pressure in hypertensive rats.
Computational docking suggests select ACEi peptides may activate ACE2; leaves open in vivo cardiovascular effects.
Angiotensin-converting enzyme (ACE) catalyzes the formation of angiotensin II (Ang II), a vasoconstrictor, whereas its homologue ACE2 degrades Ang II into angiotensin (1-7) (Ang (1-7)), a vasodilator. Given the similarities in structure and their interconnected roles in the regulation of cardiovascular system, this study aims to investigate if ACE-inhibitory (ACEi) peptides can also activate ACE2. About 200 potent ACEi peptides were subjected to molecular docking, 20 peptides were selected for cell and in vitro enzymatic activity studies, and 5 peptides were fed orally to spontaneously hypertensive rats at a dose of 15 mg/kg body weight/day for 7 days. Peptides IKW and RIY showed significant antihypertensive activity with activated circulating/aortic ACE2, circulating Ang (1-7), and decreased Ang II levels. IQY reduced blood pressure, increased Ang (1-7) level, but did not affect ACE and ACE2. Peptides MAW and MRW did not affect blood pressure, ACE, and ACE2. Our study showed that ACE2 activation is not a common feature of ACEi peptides.
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Wang et al. (2023) studied Hypertension (spontaneously hypertensive rats). ACE-inhibitory peptides (IKW, RIY, IQY, MAW, MRW) was evaluated on ACE2 activation and blood pressure reduction. ACE2 activation is not a common feature of ACE-inhibitory peptides, although specific peptides like IKW and RIY showed significant antihypertensive activity with activated ACE2.
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